Chemical Probes logo
Sivopixant | Antagonist of P2RX3
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
P2RX3
    • IC50:4.2 nM (human)
    • IC50:4.0 nM (rat)
    Antagonist
    100 nM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    In cell inhibitory activity IC50 >30000 nM for P2X1, P2X2, P2X4, P2X7 while P2X2/3 had IC50 1100 nM ...

    Potency
    Cellular
    In Vitro

    P2RX3

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.bmcl.2021.128384

    In Vivo Validations

    Rat
    Dose: 1 mg/kg
    Route of delivery: Intravenous
    Plasma half life: 10.1 h
    Systemic clearance: 2.7 mL/min/kg
    Fb : 99 %

    DOI Reference: 10.1016/j.bmcl.2021.128384

    Dose: 3 mg/Kg
    Route of delivery: Oral
    Cmax: 1630 ng/mL
    Area Under the Curve:: 14000 ng*hr/mL
    Bioavailability: 76.8 %
    Target engagement assay: strong analgesic effect in the rat Seltzer model of allodynia (ED50 0.4 mg/kg)

    DOI Reference: 10.1016/j.bmcl.2021.128384

    Chemical Information

    Molecular Formula C25H22ClN5O5
    SMILEs C[C@@H](Cn1c(=O)nc(Nc2ccc(Oc3ccccn3)cc2)n(Cc2ccc(Cl)cc2)c1=O)C(=O)O
    InChI InChI=1S/C25H22ClN5O5/c1-16(22(32)33)14-31-24(34)29-23(30(25(31)35)15-17-5-7-18(26)8-6-17)28-19-9-11-20(12-10-19)36-21-4-2-3-13-27-21/h2-13,16H,14-15H2,1H3,(H,32,33)(H,28,29,34)/t16-/m0/s1
    Molecular weight 507.13 Da
    AlogP 0.0
    HBond acceptors 10
    HBond donors 2
    Atoms 58

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    No SERP comments found for Sivopixant

    Probe Sivopixant is in the process of SERP review.

    Please continue to check back for new reviews and commentary.